Fareston Toremifene Citrate
Pharmaceutical Name: Toremifene Citrate
Drug Class: Selective Estrogen Receptor Modulator
Active Life: 5-7 days
Toremifene citrate is a non-steroidal triphenylethylene derivative that
exhibits anti-estrogenic properties. It acts as an estrogen receptor
antagonist and is quite comparable to tamoxifen citrate in both its actions
and mechanisms by which they work. However it is the apparent improved safety
of use that toremifene citrate offers that is the main benefit behind it for
strength athletes, bodybuilders and other steroid users. Medically, toremifene
citrate was developed and is still used to treat breast cancer and was first
approved by the Food and Drug Administration for this use in the United States
Similar to the other more commonly used selective estrogen receptor modulators
used by steroids users, namely clomiphene citrate and tamoxifen citrate, the
toremifene citrate molecule binds to estrogen receptors. Thus this leads to
the estrogen being blocked from interacting with the receptor and it can not
have any influence thereby remaining inactive in that tissue. By doing so an
"anti-estrogenic" effect is achieved.
The difficulty in using toremifene citrate is the lack of research conducted
using human subjects, and specifically male subjects. While it is possible to
apply most of what is known about the other selective estrogen receptor
modulators to toremifene citrate, independent research conducted with the drug
itself is invaluable and therefore a risk is taken when using the drug because
of the lack of information. Unfortunately toremifene citrate is possibly the
least researched selective estrogen receptor modulator, with the possible
exception of Raloxifene.
Despite the lack of human-based research available, in terms of its use in
steroid users, toremifene citrate can help in two ways. Firstly due to the
binding affinity of the compound it is able to help in the prevention of
gynocomastia. Toremifene citrate will compete with estrogen for the estrogen
receptors in certain tissues, including the breast, and if it can bind to the
receptor estrogen will not have an opportunity to interact with receptor and
therefore gynocomastia should not be able to develop. When using anabolic
steroids that can convert to estradiol (estrogen) this protection against
gynocomastia can be invaluable. However it should be noted that toremifene
citrate will not eliminate the estrogen or disallow the conversion to occur.
Instead it attempts to counteract the effects of circulating estrogen in the
body in those tissues that the drug effects. Therefore there is no evidence
that toremifene citrate has any effects counteracting estrogenic side effects
that are unrelated to the tissues not affected by the drug. Namely there is no
real causal connection to any reduction in water retention and acne in users
that begin taking toremifene citrate as it relates to estrogen.
The second, and possibly more beneficial, aspect of toremifene citrate for
steroid users is its ability to increase the production of luteinizing hormone
and follicle stimulating hormone, and therefore increasing testosterone. This
ability is why it is often used by steroid users during their post-cycle
therapy. Toremifene citrate would accomplish this by blocking the negative
feedback inhibition caused by estrogen at the hypothalamus and pituitary, and
this in turn will help to increase the production of these hormones. Currently
there is no available research that directly links toremifene citrate to being
able to raise testosterone levels in male users, however due to the nearly
identical mechanisms that both tamoxifen and toremifene citrate use and the
reactions that they produce in the body, it would be easy to extrapolate that
both drugs should have similar effects in this respect as well. Anecdotally
users have reported good results with toremifene citrate and say that they are
at least comparable that those of tamoxifen citrate.
One area where it has seemingly been demonstrated that toremifene citrate
outperforms tamoxifen citrate is in terms of its positive effects on the
regulation of serum cholesterol (1, 2). It has been shown that toremifene
citrate not only supports HDL synthesis, but also LDL reductions. This is due
to the estrogenic action of the drug in the liver. While there is some
evidence that tamoxifen citrate produces a somewhat similar response, this is
significantly outweighed by the response produced by toremifene citrate. It
appears that toremifene citrate would be a solid addition for cholesterol
support during an anabolic steroid cycle, where the results produced by
tamoxifen citrate in the available research are sometimes less then
In terms of dosing, sixty milligrams of toremifene citrate has been shown to
be similar in effect to that of approximately twenty milligrams of tamoxifen
citrate in terms of estrogen receptor binding ability (3). From this it can be
extrapolated that for treatment and/or prevention of gynocomastia sixty
milligrams should be sufficient for treatment. The same could be said for use
during post-cycle therapy when the user wants to raise his testosterone levels
as quickly as possible. However, as stated earlier in this profile, no
research is currently available that definitively states that there is a
certain dosage of the drug that does indeed raise testosterone levels in users
whose are suppressed.
In terms of dosing frequency, the drug has a fairly long active life therefore
one could administer the compound once every few days. However to maintain
fairly stable levels of the drug circulating in their system most users would
be best served to administer the drug at least every other day or ideally
every day. This ensures that there are no extreme spikes in the level of the
drug and no severe tapering off.
In terms of the safety of toremifene citrate, there is some evidence that
suggests that it is actually safer and presents less possible serious side
effects then tamoxifen citrate (4). For example the risk of stroke, pulmonary
embolism, and cataract are all lower when using toremifene citrate when
compared to that of tamoxifen citrate (5), although the incident of ocular
toxicity is fairly rare with both drugs (6).
There is no toxicity issues directly related to the use of toremifene citrate
(2, 7). Any issues arising in this area were seemingly caused by the hormonal
effects of the drug, rather then the properties of the drug itself. As well,
most of these complications were connected to the disease, namely breast
cancer, that the drug was being administered to treat. For the purposes of
anabolic steroid users, toremifene citrate poses no potential toxicity issues.
The only major concern is that there is no available research on the long term
effects of administration of this drug. Of course this is due to the drug only
having been approved for use since the mid-1990s. Outside of these concerns
however, it appears that toremifene is a relatively safe compound for use by
most anabolic steroid users.
1. Saarto T, Blomqvist C, Ehnholm C, Taskinen MR, Elomaa I.
Antiatherogenic effects of adjuvant antiestrogens: a randomized trial
comparing the effects of tamoxifen and toremifene on plasma lipid levels in
postmenopausal women with node-positive breast cancer. J Clin Oncol. 1996
2. Kusama M, Miyauchi K, Aoyama H, Sano M, Kimura M, Mitsuyama S, Komaki K,
Doihara H. Effects of toremifene (TOR) and tamoxifen (TAM) on serum lipids in
postmenopausal patients with breast cancer. Breast Cancer Res Treat. 2004
3. Valavaara R, Pyrhonen S, Heikkinen M, Rissanen P, Blanco G, Tholix E,
Nordman E, Taskinen P, Holsti L, Hajba A. Toremifene, a new antiestrogenic
compound, for treatment of advanced breast cancer. Phase II study. Eur J
Cancer Clin Oncol. 1988 Apr;24(4):785-90.
4. Riggs BL, Hartman L. Selective estrogen-receptor modulators -- mechanism of
action and application to clinical practice. N Engl J Med. 2003;348:618-629.
5. Harvey HA, Kimura M, Hajba A. Toremifene: An evaluation of its safety
profile. Breast. 2005 Nov 8
6. Gianni L, Panzini I, Li S, Gelber RD, Collins J, Holmberg SB, Crivellari D,
Castiglione-Gertsch M, Goldhirsch A, Coates AS, Ravaioli A; International
Breast Cancer Study Group (IBCSG). Ocular toxicity during adjuvant
chemoendocrine therapy for early breast cancer: results from International
Breast Cancer Study Group trials. Cancer. 2006 Feb 1;106(3):505-13.
7. Gong C, Song E, Jia W, Qin L, Guo J, Jia H, Hu X, Su F. A double-blind
randomized controlled trial of toremifen therapy for mastalgia. Arch Surg.
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